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Possibility of Sublingual Mono Therapy

Is it possible for somebody to achieve testosterone suppression through sublingual Estradiol tablets? I know that in theory you should be able to just take several tablets a day but I was wondering if anybody else had chosen this route?

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  • Sublingual results in some still being swallowed, so one concern is about putting really high doses on the liver. There is also just the logistical difficulty of dosing frequently enough to keep your levels high enough, there is less margin for error.

    Why not injections for monotherapy?

    • What about patches? That should spread it out.

      • What I've heard about patches is that it can be difficult to get your estrogen high enough with them (for monotherapy at least). I've also heard other problems like rashes, the patches falling off too early (and being expensive to replace), and needing too many to make monotherapy reasonable.

        Again, why not injections?

    • I just started HRT, Oral 2MG estradiol. I was just curious because I know that most of the sublingual meds are supposed to go directly into your blood stream and what heads to your liver should be minimal, as opposed to oral where the dose has to be high enough to pass through your liver.

      I think I'm willing to pop them like tic tacs if needed. Image

      • Sublingual might have better absorption than oral, but that isn't saying much and you are still swallowing some of the dose. I still think the dose you would need to do monotherapy is more than is reasonable for oral or sublingual routes of administration.

        Also, it's not just how many pills you would need to take to keep up your levels, but the exact timing. It also means all day you are constantly having sharp increases and decreases in your hormone levels. It's impractical for lots of reasons.

        Injections are ideal for monotherapy, but if that's not an option I would stick to more typical doses of sublingual estrogen and an anti-androgen (though the anti-androgens can have side effects). Patches and gel are better for absorption than oral (most of the estrogen is absorbed by the liver, little of your dose gets into the bloodstream - it's really the worst route of administration), but they have their own logistical problems.

        I highly recommend reading this: https://transfemscience.org/articles/transfem-intro/

  • https://www.liebertpub.com/doi/10.1089/trgh.2023.0022

    this study that compares the differences between sublingual monotherapy, and oral estradiol in combination with cyproterone acetate. this is their conclusion.

    Both treatments achieved similar clinical changes. At this stage, (sublingual estradiol), which repeatedly induces alarming excursions of serum estradiol throughout the day, appears to offer no advantage over the cyproterone acetate approach.

    my conclusion from this is that you should only attempt sublingual monotherapy if it is cheaper and/or easier to obtain the larger amount of estradiol you need, than the lower dose of estradiol with some way to block t.

  • scientifically possible? yes

    is it worth doing? probably not

  • injections are scary but you get used to them. I was doing 8mg sublingual for years and eventually did stop taking spiro (only after a few years), but injections are just so much more convenient.

  • I was able to do it. Since sublingual has a fast half life you'll need to spread the doses throughout the day as many times as you can. For me the bare minimum was 1mg every six hours for a total of 4mg each day though my body is pretty sensitive to estradiol overall. (The last pill I'd take directly before bed so I'd be sleeping more than 6 hours)

    I do think it helps to start off slow and ramp things up over time so that your body adapts but that is anecdotal on my end and mostly theory on the research side. Also if you're able to get injections or tolerate an androgen suppressor it's much easier than doing sublingual 4 times a day

    • Did you get tablets formulated for sublingual or did you have to dissolve oral tablets under your tongue?

      • Most tablets can be used sublingually as long as they don't have a hard shell on the outside. You can dissolve them under your tongue, under your lip, or in your cheek. Personally I like to keep them behind my bottom lip.

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